[go: up one dir, main page]

EP1309322A2 - Procede pour traiter des troubles neurodegeneratifs de la retine et de la papille optique - Google Patents

Procede pour traiter des troubles neurodegeneratifs de la retine et de la papille optique

Info

Publication number
EP1309322A2
EP1309322A2 EP01959734A EP01959734A EP1309322A2 EP 1309322 A2 EP1309322 A2 EP 1309322A2 EP 01959734 A EP01959734 A EP 01959734A EP 01959734 A EP01959734 A EP 01959734A EP 1309322 A2 EP1309322 A2 EP 1309322A2
Authority
EP
European Patent Office
Prior art keywords
substitution
branched alkyl
derivative
amino
benzoylphenylacetic acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP01959734A
Other languages
German (de)
English (en)
Other versions
EP1309322B1 (fr
Inventor
Daniel A. Gamache
Gustav Graff
John M. Yanni
Michael A. Kapin
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alcon Inc
Original Assignee
Alcon Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Alcon Inc filed Critical Alcon Inc
Publication of EP1309322A2 publication Critical patent/EP1309322A2/fr
Application granted granted Critical
Publication of EP1309322B1 publication Critical patent/EP1309322B1/fr
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • This invention relates to the treatment of retinopathy.
  • this invention relates to the use of certain 3-benzoylphenylacetic acids and derivatives to treat or prevent neurodegenerative disorders of the retina and optic nerve head.
  • 3-benzoylphenylacetic acid and certain of its derivatives are known to possess anti-inflammatory activity.
  • U.S. Patent Nos. 4,254,146, 4,045,576, 4,126,635, and 4,503,073, and U.K. Patent Application Nos. 2,071 ,086A and 2,093,027A disclose various 3-benzoylphenylacetic acids, salts and esters, and hydrates thereof, having anti-inflammatory activity.
  • U.S. Patent No. 4,568,695 discloses 2-amino-3-benzoylphenylethyl alcohols having anti-inflammatory activity.
  • U.S. Patent No. 4,313,949 discloses 2-amino-3-benzoyl- phenylacetamides having anti-inflammatory activity.
  • U.S. patent No. 4,683,242 teaches the transdermal administration of 2- amino-3-benzoylphenylacetic acids, salts, and esters, and hydrates and alcoholates thereof to control inflammation and alleviate pain.
  • U.S. Patent No. 4,910,225 teaches certain benzoylphenylacetic acids for local administration to control ophthalmic, nasal or otic inflammation. Only acetic acids are disclosed in the '225 patent; no esters or amides are mentioned or taught as anti-inflammatory agents for local administration to the eyes, nose and ears.
  • U.S. Patent No. 5,475,034 discloses topically administrable compositions containing certain amide and ester derivatives of 3- benzyolphenylacetic acid, including nepafenac, useful for treating ophthalmic inflammatory disorders and ocular pain.
  • nepafenac nepafenac
  • [s]uch disorders include, but are not limited to uveitis, scleritis, episcleritis, keratitis, surgically-induced inflammation and endophthalmitis.”
  • U.S. Patent No. 6,066,671 discloses the topical use of certain amide and ester derivatives of 3-benzoylphenylacetic acid, including nepafenac, for treating GLC1 A glaucoma.
  • 3-benzoylphenylacetic acids and derivatives including nepafenac (2-amino,3-benzoyl-phenylacetamide), are useful in treating neurodegenerative disorders of the retina and optic nerve head.
  • 3-benzoylphenylacetic acids and derivatives useful in the methods of the present invention are those of formula (I) below.
  • R H, C 1-4 (un)branched alkyl, CF 3) SR 4
  • R' H, Ci-io (un)branched alkyl, (un)substituted (substitution as defined by X below), (un)substituted heterocycle (substitution as defined by X below),
  • R 3 H, Ci_ 6 (un)branched alkyl, (un)substituted aryl (substitution as defined by X below), (un)substituted heterocycle (substitution as defined by X below)
  • A H, OH, optionally (un)substituted aryl (substitution as defined by X below), (un)substituted heterocycle (substitution as defined by X below), — (CH 2 ) ⁇ OR 3 ;
  • Preferred compounds for use in the methods of the present invention are those of Formula I wherein:
  • R H, d. 2 alkyl
  • Y NR'R";
  • R' H, C 1-6 (un)branched alkyl, — (CH 2 ) dislikeZ(CH 2 ) awkwardA;
  • Z nothing, O, CHOR 3 , NR 3 ;
  • the most preferred compounds for use in the compositions or method of the present invention are 2-Amino-3-(4-fluorobenzoyl)-phenylacetamide; 2- Amino-3-benzoyl-phenylacetamide (nepafenac); and 2-Amino-3-(4- chlorobenzoyl)-phenylacetamide.
  • a therapeutically effective amount of a compound of formula (I) is administered topically, locally or systemically to treat or prevent neurodegenerative disorders of the retina and optic nerve head.
  • Such disorders include, but are not limited to atrophic macular degeneration; retinitis pigmentosa; iatrogenic retinopathy; retinal tears and holes; diabetic retinopathy; sickle cell retinopathy; retinal vein and artery occlusion; and optic neuropathy.
  • Certain ophthalmic disorders such as sickle cell retinopathy and retinal vein or artery occlusion, can be characterized by both angiogenesis and neurodegenerative components.
  • a compound of formula (I) is administered to treat or prevent disorders characterized, at least in part, by neurodegeneration.
  • the compounds of formula (I) can be administered in a variety of ways, including all forms of local delivery to the eye, such as subconjunctival injections or implants, intravitreal injections or implants, sub-Tenon's injections or implants, incorporation in surgical irrigating solutions, etc. Additionally, the compounds of formula (I) can be administered systemically, such as orally or intravenously. Suitable pharmaceutical vehicles or dosage forms for injectable compositions, implants, and systemic administration are known.
  • compositions comprising a compound of formula (I) in aqueous solution or suspension, optionally containing a preservative for multidose use and other conventionally employed ophthalmic adjuvants, can be topically administered to the eye.
  • the most preferred form of delivery is by aqueous eye drops, but gels or ointments can also be used.
  • Aqueous eye drops, gels and ointments can be formulated according to conventional technology and would include one or more excipients.
  • topically administrable compositions may contain tonicity-adjusting agents, such as mannitol or sodium chloride; preservatives such as chlorobutanol, benzalkonium chloride, polyquatemium-1 , or chlorhexidine; buffering agents, such as phosphates, borates, carbonates and citrates; and thickening agents, such as high molecular weight carboxy vinyl polymers, including those known as carbomers, hydroxyethylcellulose, or polyvinyl alcohol.
  • tonicity-adjusting agents such as mannitol or sodium chloride
  • preservatives such as chlorobutanol, benzalkonium chloride, polyquatemium-1 , or chlorhexidine
  • buffering agents such as phosphates, borates, carbonates and citrates
  • thickening agents such as high molecular weight carboxy vinyl polymers, including those known as carbomers, hydroxyethylcellulose, or polyvinyl alcohol.
  • compositions intended for topical ophthalmic administration will typically contain a compound of formula (I) in an amount of from about 0.001 to about 4.0% (w/v), preferably from about 0.01 to about 0.5% (w/v), with 1-2 drops once to several times a day.
  • representative doses for other forms of preparations are approximately 1 - 100 mg/day/adult for injections and approximately 10 - 1000 mg/adult for oral preparations, each administered once to several times a day.
  • Additional therapeutic agents may be added to supplement the compounds of formula (I).
  • Example 1 The following formulations are representative of the topical compositions useful in the present invention.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne l'utilisation d'acides 3-benzolphénylacétiques, notamment de népafénac, afin de traiter des troubles neurodégénératifs de la rétine.
EP01959734A 2000-08-14 2001-08-13 Utilisation therapeutique de derives d'acide 3-benzoylphenylacetique pour traiter les affections de la retine Expired - Lifetime EP1309322B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22513200P 2000-08-14 2000-08-14
US225132P 2000-08-14
PCT/US2001/025319 WO2002013805A2 (fr) 2000-08-14 2001-08-13 Procede pour traiter des troubles neurodegeneratifs de la retine et de la papille optique

Publications (2)

Publication Number Publication Date
EP1309322A2 true EP1309322A2 (fr) 2003-05-14
EP1309322B1 EP1309322B1 (fr) 2006-06-21

Family

ID=22843666

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01959734A Expired - Lifetime EP1309322B1 (fr) 2000-08-14 2001-08-13 Utilisation therapeutique de derives d'acide 3-benzoylphenylacetique pour traiter les affections de la retine

Country Status (16)

Country Link
US (1) US6638976B2 (fr)
EP (1) EP1309322B1 (fr)
JP (1) JP2004506010A (fr)
AR (1) AR030346A1 (fr)
AT (1) ATE330596T1 (fr)
AU (1) AU8125801A (fr)
BR (1) BR0113201A (fr)
CA (1) CA2418059C (fr)
CY (1) CY1106155T1 (fr)
DE (1) DE60120990T2 (fr)
DK (1) DK1309322T3 (fr)
ES (1) ES2266229T3 (fr)
MX (1) MXPA03001160A (fr)
PT (1) PT1309322E (fr)
TW (1) TWI286933B (fr)
WO (1) WO2002013805A2 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040132773A1 (en) * 2001-08-13 2004-07-08 Gamache Daniel A Method of treating neurodgenerative disorders of the retina and optic nerve head
JP2007500250A (ja) * 2003-06-13 2007-01-11 アルコン，インコーポレイテッド 病的な眼の新脈管形成を処置するための非ステロイド性抗炎症剤の処方物
US20050009910A1 (en) * 2003-07-10 2005-01-13 Allergan, Inc. Delivery of an active drug to the posterior part of the eye via subconjunctival or periocular delivery of a prodrug
TWI358290B (en) 2004-12-02 2012-02-21 Alcon Inc Topical nepafenac formulations
BRPI0608774A2 (pt) * 2005-05-10 2010-01-26 Alcon Inc composição de suspensão oftálmica aquosa topicamente administrável e uso da mesma
US20060257487A1 (en) * 2005-05-10 2006-11-16 Alcon, Inc. Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders
US9370444B2 (en) 2010-10-12 2016-06-21 Emmett T. Cunningham, JR. Subconjunctival conformer device and uses thereof
US8915877B2 (en) 2010-10-12 2014-12-23 Emmett T. Cunningham, JR. Glaucoma drainage device and uses thereof
RU2458656C1 (ru) * 2011-06-17 2012-08-20 Федеральное государственное учреждение "Межотраслевой научно-технический комплекс "Микрохирургия глаза" имени академика С.Н. Федорова Федерального агентства по высокотехнологичной медицинской помощи" Способ лечения оперированного незакрывшегося макулярного отверстия
EP3013790A1 (fr) 2013-06-27 2016-05-04 Mylan Laboratories Ltd. Procédé pour la préparation de népafénac

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1226344A (fr) 1967-07-31 1971-03-24
SE400966B (sv) * 1975-08-13 1978-04-17 Robins Co Inc A H Forfarande for framstellning av 2-amino-3-(eller 5-)bensoyl-fenylettiksyror
US4313949A (en) * 1979-09-26 1982-02-02 A. H. Robins Company, Inc. Method of producing an inhibitory effect on blood platelet aggregation
US4254146A (en) * 1979-10-18 1981-03-03 A. H. Robins Company, Inc. 3-Benzoyl-2-nitrophenylacetic acids, metal salts, amides and esters
IL61945A (en) 1980-02-19 1984-09-30 Robins Co Inc A H 2-amino-3-(hydroxy(phenyl)methyl)phenylacetic acids,esters and amides and pharmaceutical compositions containing them
DE3026402A1 (de) * 1980-07-11 1982-02-04 Syntex Corp., Palo Alto, Calif. Die verwendung analgetischer und nicht-hormonaler, entzuendungshemmender mittel bei der behandlung von mikrovaskulaeren erkrankungen
US4503073A (en) * 1981-01-07 1985-03-05 A. H. Robins Company, Incorporated 2-Amino-3-(alkylthiobenzoyl)-phenylacetic acids
IL64724A0 (en) * 1981-02-17 1982-03-31 Robins Co Inc A H 2-amino-3-(halobenzoyl)-methylphenylacetic acids and esters and salts thereof and pharmaceutical compositions containing them
US4454151A (en) 1982-03-22 1984-06-12 Syntex (U.S.A.) Inc. Use of pyrrolo pyrroles in treatment of ophthalmic diseases
US4568695A (en) 1983-12-07 1986-02-04 A. H. Robins Company, Incorporated 2-Amino-3-benzoyl-phenethylalcohols and intermediates therefor
EP0195582B1 (fr) 1985-03-14 1990-01-24 SMITH KLINE DAUELSBERG GmbH Derivés de l'acide Amino-5 salicylique d'acide anti-inflammatoires non-steroiques
US4851443A (en) 1985-03-14 1989-07-25 Smith Kline Dauelsberg, Gmbh Carboxylic acid amides, compositions and medical use thereof
US4683242A (en) * 1985-10-28 1987-07-28 A. H. Robins Company, Incorporated Transdermal treatment for pain and inflammation with 2-amino-3-aroylbenzeneacetic acids, salts and esters
DK406686D0 (da) 1986-08-26 1986-08-26 Hans Bundgaard Carboxylsyrederivater
CA1325382C (fr) 1988-01-27 1993-12-21 Takahiro Ogawa Composition therapeutique a administration locale pour les affections inflammatoires
US5314909A (en) 1993-03-17 1994-05-24 Merck & Co., Inc. Use of non-steroidal antiiflammatory agents in macular degeneration
JP3396953B2 (ja) 1994-05-10 2003-04-14 千寿製薬株式会社 網膜疾患予防・治療剤
US5475034A (en) * 1994-06-06 1995-12-12 Alcon Laboratories, Inc. Topically administrable compositions containing 3-benzoylphenylacetic acid derivatives for treatment of ophthalmic inflammatory disorders
US5643943A (en) * 1994-12-23 1997-07-01 Alcon Laboratories, Inc. Systemic administration of esters and amides of antioxidants which may be used as antioxidant prodrug therapy for oxidative and inflammatory pathogenesis
US5811446A (en) * 1997-04-18 1998-09-22 Cytos Pharmaceuticals Llc Prophylactic and therapeutic methods for ocular degenerative diseases and inflammations and histidine compositions therefor
US6025353A (en) 1997-11-19 2000-02-15 G.D. Searle & Co. Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents
US6066671A (en) 1997-12-19 2000-05-23 Alcon Laboratories, Inc. Treatment of GLC1A glaucoma with 3-benzoyl-phenylacetic acids, esters, or amides
IL144126A0 (en) 1999-01-07 2002-05-23 Univ Vanderbilt A method of altering the specificity of cyclooxygenase-inhibiting compounds
US6555540B1 (en) 1999-06-30 2003-04-29 Pfizer Inc Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
US6413965B1 (en) 1999-06-30 2002-07-02 Pfizer Inc. Compositions and treatment for diabetic complications
US6426341B1 (en) 1999-06-30 2002-07-30 Pfizer Inc. Treatment for diabetic complications
US6416777B1 (en) 1999-10-21 2002-07-09 Alcon Universal Ltd. Ophthalmic drug delivery device

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0213805A2 *

Also Published As

Publication number Publication date
CY1106155T1 (el) 2011-06-08
ATE330596T1 (de) 2006-07-15
DE60120990T2 (de) 2007-03-15
US6638976B2 (en) 2003-10-28
US20020049255A1 (en) 2002-04-25
BR0113201A (pt) 2006-05-09
TWI286933B (en) 2007-09-21
HK1057332A1 (en) 2004-04-02
JP2004506010A (ja) 2004-02-26
ES2266229T3 (es) 2007-03-01
DK1309322T3 (da) 2006-10-23
MXPA03001160A (es) 2004-08-02
DE60120990D1 (de) 2006-08-03
WO2002013805A2 (fr) 2002-02-21
AU8125801A (en) 2002-02-25
WO2002013805A3 (fr) 2002-05-30
PT1309322E (pt) 2006-11-30
CA2418059C (fr) 2009-12-22
AR030346A1 (es) 2003-08-20
EP1309322B1 (fr) 2006-06-21
CA2418059A1 (fr) 2002-02-21

Similar Documents

Publication Publication Date Title
JP2012193214A (ja) ベンゾイルフェニル酢酸を使用して、血管形成関連障害を処置するための方法
HK1211216A1 (en) Non-irritating ophthalmic povidone-iodine compositions
EP2734206A1 (fr) Combinaison à dose fixe de bimatoprost et brimonidine
US6638976B2 (en) Method of treating neurodegenerative disorders of the retina and optic nerve head
AU2001283337A1 (en) Method of treating angiogenesis-related disorders using benzoyl phenylacetic acid
US6646003B2 (en) Method of treating ocular inflammatory and angiogenesis-related disorders of the posterior segment of the eye using an amide derivative of flurbiprofen or ketorolac
US20040132773A1 (en) Method of treating neurodgenerative disorders of the retina and optic nerve head
AU2001281258B2 (en) Method of treating neurodegenerative disorders of the retina and optic nerve head
JP2004506010A5 (fr)
US20030207941A1 (en) Method of treating vascular endothelial growth factor mediated vascular disorders
AU2001281258A1 (en) Method of treating neurodegenerative disorders of the retina and optic nerve head
US20030187072A1 (en) Method of treating angiogenesis-related disorders
HK1057332B (en) Use of 3-benzoylphenylacetic acid derivatives for the treatment of retinal disorders
HK1057331B (en) Treatment of angiogenesis-related disorders using benzoyl phenylacetic acid derivatives
AU2006217547A1 (en) Method of treating angiogenesis-related disorders
JP2020514347A (ja) チオトロピウムを有効成分として含有する近視予防、近視治療および／または近視進行抑制剤
JP2003505499A (ja) 緑内障の治療のための２−アミノテトラリン誘導体
EP0607697A2 (fr) DILAZEP pour la réduction de la pression intraoculaire élevée

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20030207

AK Designated contracting states

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

AX Request for extension of the european patent

Extension state: AL LT LV MK RO SI

17Q First examination report despatched

Effective date: 20040318

RAP1 Party data changed (applicant data changed or rights of an application transferred)

Owner name: ALCON, INC.

RTI1 Title (correction)

Free format text: USE OF 3-BENZOYLPHENYLACETIC ACID DERIVATIVES FOR THE TREATMENT OF RETINAL DISORDERS

GRAP Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOSNIGR1

RIC1 Information provided on ipc code assigned before grant

Ipc: A61P 27/02 20060101ALI20051222BHEP

Ipc: A61K 31/215 20060101AFI20051222BHEP

Ipc: A61K 31/165 20060101ALI20051222BHEP

Ipc: A61P 25/02 20060101ALI20051222BHEP

Ipc: A61K 31/185 20060101ALI20051222BHEP

GRAS Grant fee paid

Free format text: ORIGINAL CODE: EPIDOSNIGR3

GRAA (expected) grant

Free format text: ORIGINAL CODE: 0009210

AK Designated contracting states

Kind code of ref document: B1

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

REG Reference to a national code

Ref country code: GB

Ref legal event code: FG4D

REG Reference to a national code

Ref country code: CH

Ref legal event code: EP

REG Reference to a national code

Ref country code: IE

Ref legal event code: FG4D

REF Corresponds to:

Ref document number: 60120990

Country of ref document: DE

Date of ref document: 20060803

Kind code of ref document: P

REG Reference to a national code

Ref country code: SE

Ref legal event code: TRGR

REG Reference to a national code

Ref country code: DK

Ref legal event code: T3

REG Reference to a national code

Ref country code: GR

Ref legal event code: EP

Ref document number: 20060403112

Country of ref document: GR

REG Reference to a national code

Ref country code: PT

Ref legal event code: SC4A

Free format text: AVAILABILITY OF NATIONAL TRANSLATION

Effective date: 20060914

ET Fr: translation filed
REG Reference to a national code

Ref country code: ES

Ref legal event code: FG2A

Ref document number: 2266229

Country of ref document: ES

Kind code of ref document: T3

PLBE No opposition filed within time limit

Free format text: ORIGINAL CODE: 0009261

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: NO OPPOSITION FILED WITHIN TIME LIMIT

REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1057332

Country of ref document: HK

26N No opposition filed

Effective date: 20070322

REG Reference to a national code

Ref country code: FR

Ref legal event code: PLFP

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: LU

Payment date: 20160801

Year of fee payment: 16

Ref country code: NL

Payment date: 20160810

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: CH

Payment date: 20160812

Year of fee payment: 16

Ref country code: DE

Payment date: 20160809

Year of fee payment: 16

Ref country code: GB

Payment date: 20160810

Year of fee payment: 16

Ref country code: MC

Payment date: 20160712

Year of fee payment: 16

Ref country code: FI

Payment date: 20160809

Year of fee payment: 16

Ref country code: IT

Payment date: 20160822

Year of fee payment: 16

Ref country code: DK

Payment date: 20160810

Year of fee payment: 16

Ref country code: IE

Payment date: 20160809

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: AT

Payment date: 20160725

Year of fee payment: 16

Ref country code: PT

Payment date: 20160811

Year of fee payment: 16

Ref country code: GR

Payment date: 20160722

Year of fee payment: 16

Ref country code: CY

Payment date: 20160705

Year of fee payment: 16

Ref country code: FR

Payment date: 20160712

Year of fee payment: 16

Ref country code: SE

Payment date: 20160811

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: TR

Payment date: 20160719

Year of fee payment: 16

Ref country code: BE

Payment date: 20160713

Year of fee payment: 16

Ref country code: ES

Payment date: 20160712

Year of fee payment: 16

REG Reference to a national code

Ref country code: DE

Ref legal event code: R119

Ref document number: 60120990

Country of ref document: DE

REG Reference to a national code

Ref country code: DK

Ref legal event code: EBP

Effective date: 20170831

REG Reference to a national code

Ref country code: CH

Ref legal event code: PL

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: MC

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

REG Reference to a national code

Ref country code: NL

Ref legal event code: MM

Effective date: 20170901

REG Reference to a national code

Ref country code: AT

Ref legal event code: MM01

Ref document number: 330596

Country of ref document: AT

Kind code of ref document: T

Effective date: 20170813

GBPC Gb: european patent ceased through non-payment of renewal fee

Effective date: 20170813

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: FI

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: SE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170814

Ref country code: LI

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

Ref country code: CY

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: CH

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

REG Reference to a national code

Ref country code: FR

Ref legal event code: ST

Effective date: 20180430

REG Reference to a national code

Ref country code: IE

Ref legal event code: MM4A

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: GR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20180305

Ref country code: AT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: PT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20180214

REG Reference to a national code

Ref country code: BE

Ref legal event code: MM

Effective date: 20170831

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LU

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: NL

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170901

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: DK

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

Ref country code: DE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20180301

Ref country code: GB

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: IE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: IT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813

Ref country code: FR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

Ref country code: BE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170831

REG Reference to a national code

Ref country code: ES

Ref legal event code: FD2A

Effective date: 20181025

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: ES

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170814

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: TR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20170813